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公开(公告)号：US20110182855A1
公开(公告)日：2011-07-28
申请号：US13077980
申请日：2011-03-31
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译： 通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自经由亲核部分与A和B连接; 或Z 1和Z 2一起表示衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子缀合而形成。
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公开(公告)号：US07939630B2
公开(公告)日：2011-05-10
申请号：US12458931
申请日：2009-07-28
IPC分类号： C07K1/13
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译： 通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自经由亲核部分与A和B连接; 或Z 1和Z 2一起表示衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子缀合而形成。
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公开(公告)号：US08816051B2
公开(公告)日：2014-08-26
申请号：US13077980
申请日：2011-03-31
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译： 通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自经由亲核部分与A和B连接; 或Z 1和Z 2一起表示衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子结合而形成。
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公开(公告)号：US20090298154A1
公开(公告)日：2009-12-03
申请号：US12458931
申请日：2009-07-28
IPC分类号： C12N9/96 , C07C321/24 , C07K17/00 , C07K1/00
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
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公开(公告)号：US07595292B2
公开(公告)日：2009-09-29
申请号：US10564340
申请日：2004-07-12
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W- together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译： 通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自经由亲核部分与A和B连接; 或Z 1和Z 2一起表示衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子缀合而形成。
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公开(公告)号：US20060210526A1
公开(公告)日：2006-09-21
申请号：US10564340
申请日：2004-07-12
申请人： Stephen Brocchini , Antony Godwin , Elisa Pedone , Jin-Won Choi , Sunil Shaunak
发明人： Stephen Brocchini , Antony Godwin , Elisa Pedone , Jin-Won Choi , Sunil Shaunak
IPC分类号： A61K38/16 , A61K31/785 , C08G63/91 , C08G63/48
CPC分类号： A61K47/48215 , A61K47/60
摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W- together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.
摘要翻译： 通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自通过亲核部分连接到A和B; 或Z 1和Z 2一起代表衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子缀合而形成。
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公开(公告)号：US20090176866A1
公开(公告)日：2009-07-09
申请号：US10585286
申请日：2005-01-07
申请人： Sunil Shaunak , Stephen Brocchini , Antony Godwin , Ji-Won Choi
发明人： Sunil Shaunak , Stephen Brocchini , Antony Godwin , Ji-Won Choi
IPC分类号： A61K31/365
CPC分类号： A61K45/06 , A61K31/7048 , A61K31/78 , Y02A50/387 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415 , Y02A50/423 , Y02A50/463 , Y02A50/465 , Y02A50/471 , Y02A50/481 , Y02A50/483
摘要： A complex that comprises a narrow molecular weight distribution polymer that includes units derived from an acrylic acid or a salt thereof, and (i) a substance that has pharmacological activity against a pathogenic organism, or (ii) a substance that has pharmacological activity against a cancer, or (iii) one or more agents selected from antigens and immunogens is useful in treating and/or inducing immunity to the pathogenic organism or the cancer, and for inducing immunity to the antigen or immunogen.
摘要翻译： 一种复合物，其包含窄分子量分布聚合物，其包含衍生自丙烯酸或其盐的单元，和（i）对致病性生物体具有药理活性的物质，或（ii）具有针对病原体的药理活性的物质 癌症，或（iii）选自抗原和免疫原的一种或多种药物可用于治疗和/或诱导对致病生物体或癌症的免疫，以及诱导对抗原或免疫原的免疫。
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公开(公告)号：US20050214247A1
公开(公告)日：2005-09-29
申请号：US10511317
申请日：2003-03-18
申请人： Sunil Shaunak , Elisabetta Gianasi , Ruth Duncan
发明人： Sunil Shaunak , Elisabetta Gianasi , Ruth Duncan
IPC分类号： C07H13/02 , A61K31/7028 , A61K47/48 , A61P1/04 , A61P17/00 , A61P19/02 , A61P29/00 , A61P31/04 , A61P35/04 , A61P37/06 , C08B37/00 , C08G73/00 , A61K31/785 , C08G63/48 , C08G63/91
CPC分类号： A61K47/595
摘要： The present invention relates to new anionic glycodendrimers having new biological activity, processes for preparing them and their use in medicine including veterinary medicine.
摘要翻译： 本发明涉及具有新的生物活性的新型阴离子型糖团聚体，其制备方法及其在包括兽医学的药物中的应用。
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公开(公告)号：US20150126468A1
公开(公告)日：2015-05-07
申请号：US13818580
申请日：2011-08-22
申请人： Sunil Shaunak , Ian Alfred Teo
发明人： Sunil Shaunak , Ian Alfred Teo
IPC分类号： C07H15/26
CPC分类号： C07H15/26 , A61K47/59 , A61K47/595 , C07H5/06 , C07H11/00 , C07H13/04 , C07H15/12 , C08G73/02 , C08G73/024 , C08G73/028 , C08G83/003
摘要： A glycodendrimer comprising: a) a non-toxic dendrimer polypropyletherimine core supporting on average in the range of 9 to 64 terminal carboxylic acid groups, and b) conjugated to said core in the range of 2 to 8 amino sugars or a sulphate amino sugar selected from the group consisting of glucosamine, N-acetyl glucosamine, mannosamine, N-acetylmannosamine, galactosamine, a sulphate of any one of the same and a combination thereof, wherein each sugar is linked directly through a zero length amide bond with a residue of a terminal carboxylic acid group. The invention also extends to defined populations comprising said glycodendrimer molecules, pharmaceutical compositions comprising said molecules or populations, process for preparing the molecules and formulations, and therapeutic uses of the molecules, populations and compositions.
摘要翻译： 一种糖苷配共聚物，其包含：a）在9至64个末端羧酸基团范围内平均支持的无毒树枝状聚合物聚丙烯酰亚胺核心，b）与所述核心结合至2至8个氨基糖或选择的硫酸氨基糖 来自由葡糖胺，N-乙酰氨基葡萄糖，甘露糖胺，N-乙酰甘露糖胺，半乳糖胺，其中任何一种的硫酸盐及其组合组成的组，其中每个糖直接通过零长度的酰胺键与残基的 末端羧酸基。 本发明还延伸到包含所述糖基配体分子的定义的群体，包含所述分子或种群的药物组合物，制备分子和制剂的方法，以及分子，群体和组合物的治疗用途。
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公开(公告)号：US20130225523A1
公开(公告)日：2013-08-29
申请号：US13818557
申请日：2011-08-22
申请人： Sunil Shaunak , Ian Alfred Teo
发明人： Sunil Shaunak , Ian Alfred Teo
IPC分类号： C07H15/12
CPC分类号： C07H15/26 , A61K47/59 , A61K47/595 , C07H5/06 , C07H11/00 , C07H13/04 , C07H15/12 , C08G73/02 , C08G73/024 , C08G73/028 , C08G83/003
摘要： A glycodendrimer comprising: a) a non-toxic dendrimer polypropyletherimine core supporting 16 terminal carboxylic acid groups, and b) conjugated to said core 2, 3, 4 or 5 glucosamine molecules, wherein each glucosamine is linked directly through a zero length amide bond with a residue of a terminal carboxylic acid group. The invention also extends to defined populations comprising said glycodendrimer molecules, pharmaceutical compositions comprising said molecules or populations, process for preparing the molecules and formulations, and therapeutic uses of the molecules, populations and compositions.
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